New desulfured troglitazone derivatives: Improved synthesis and biological evaluation

Abstract : Breast cancer is a major medical threat which cannot be sufficiently addressed by current therapies because of spontaneous or acquired treatment resistance. Besides, triple-negative breast cancer (TNBC) tumors do not respond to targeted therapies, thus new therapeutic strategies are needed. In this context, we designed and prepared new desulfured troglitazone (TGZ)-derived molecules and evaluated them in vitro for their anti-proliferative activity, with a special focus on triple-negative breast cancer cell lines. Optimization of the synthetic strategies and deracemization of the lead compound were performed to give highly active compound 10 with low-micromolar potency. Further studies revealed that this compound triggers apoptosis rather than cell cycle arrest as observed with TGZ.
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Submitted on : Friday, December 20, 2019 - 11:29:49 AM
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Dorian Dupommier, Claire Muller, Corinne Comoy, Sabine Mazerbourg, Andrea Bordessa, et al.. New desulfured troglitazone derivatives: Improved synthesis and biological evaluation. European Journal of Medicinal Chemistry, Elsevier, 2020, 187, pp.111939. ⟨10.1016/j.ejmech.2019.111939⟩. ⟨hal-02421051⟩

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